Roxithromycin
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Also known as NSC-758443RoxithromycineRoxitromicinaRU 28965RU 965RU-28965RU-965Rulidroxithromycin monohydrateRoxitheromycinRoxithromicine
Summary
Roxithromycin (CHEMBL1214185) is a phase-3 clinical-stage small molecule (ATC J01FA06) targeting MLNR; indicated across 1 condition including bacterial infectious disease.
At a glance
- Status: Max clinical phase 3 (not approved)
- Modality: Small molecule
- ATC class: J01FA06
- Targets: 1 (MLNR)
- Indications: 1 condition
- Clinical trials: 5
- Chemistry: 837 Da · C41H76N2O15
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL1214185 |
| Name | Roxithromycin |
| Type | Small molecule |
| Max phase | 3 |
| FDA approved | no |
| PubChem CID | 6915744 |
| ChEBI | CHEBI:48935 |
| ATC | J01FA06 |
| Molecular formula | C41H76N2O15 |
| Molecular weight | 837 |
| InChIKey | RXZBMPWDPOLZGW-XMRMVWPWSA-N |
SMILES: CC[C@@H]1[C@@]([C@@H]([C@H](/C(=N/OCOCCOC)/[C@@H](C[C@@]([C@@H]([C@H]([C@@H]([C@H](C(=O)O1)C)O[C@H]2C[C@@]([C@H]([C@@H](O2)C)O)(C)OC)C)O[C@H]3[C@@H]([C@H](C[C@H](O3)C)N(C)C)O)(C)O)C)C)O)(C)O
IUPAC name: (3R,4S,5S,6R,7R,9R,10E,11S,12R,13S,14R)-6-[(2S,3R,4S,6R)-4-(dimethylamino)-3-hydroxy-6-methyloxan-2-yl]oxy-14-ethyl-7,12,13-trihydroxy-4-[(2R,4R,5S,6S)-5-hydroxy-4-methoxy-4,6-dimethyloxan-2-yl]oxy-10-(2-methoxyethoxymethoxyimino)-3,5,7,9,11,13-hexamethyl-oxacyclotetradecan-2-one
ChEBI definition: A major geometrical isomer of roxithromycin.
Other ChEBI roles (chemical / environmental): xenobiotic, environmental contaminant.
Also known as: NSC-758443, Roxithromycin, Roxithromycine, Roxitromicina, RU 28965, RU 965, RU-28965, RU-965, Rulid, roxithromycin, roxithromycin monohydrate, ROXITHROMYCIN
Patent coverage: 8,798 distinct patent families (25,469 SureChEMBL compound mentions), from 1 matched compound structure(s). Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.
Targets
Targets
Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).
| Gene | Target | Action | pAffinity | Cancer dependency | UniProt |
|---|---|---|---|---|---|
| MLNR | motilin receptor | Full agonist | 6.2 | 0.1% | O43193 |
Broader ChEMBL bioactivity targets: 2 (assay-derived). Sample: Motilin receptor, Alpha-1B adrenergic receptor.
Bioactivity
ChEMBL activities: 3 potent at pChembl ≥ 5 of 3 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):
| Target | pChembl | Type | Value | Unit | Activity ID |
|---|---|---|---|---|---|
| P15823 | 6.26 | Ki | 548 | nM | CHEMBL_ACT_7800576 |
| P15823 | 6 | IC50 | 989 | nM | CHEMBL_ACT_7800575 |
| MLNR | 5.05 | AC50 | 9000 | nM | CHEMBL_ACT_25189081 |
Target pathways
Aggregated over 1 target gene(s): MLNR.
Top Reactome pathways
7 total, by targets touching each:
| Pathway | Targets | Genes |
|---|---|---|
| Signal Transduction | 1 | MLNR |
| Signaling by GPCR | 1 | MLNR |
| Class A/1 (Rhodopsin-like receptors) | 1 | MLNR |
| Peptide ligand-binding receptors | 1 | MLNR |
| GPCR downstream signalling | 1 | MLNR |
| G alpha (q) signalling events | 1 | MLNR |
| GPCR ligand binding | 1 | MLNR |
Dominant GO biological processes
| GO term | Targets |
|---|---|
| G protein-coupled receptor signaling pathway | 1 |
| signal transduction | 1 |
Indications & clinical
Indications
1 indication (1 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).
| Indication | Trial phase | MONDO | EFO |
|---|---|---|---|
| bacterial infectious disease | 4 | MONDO:0005113 | EFO:0000771 |
Clinical trials
Total trials: 5.
Phase distribution
| Phase | Trials |
|---|---|
| Not specified | 2 |
| PHASE4 | 1 |
| PHASE3 | 1 |
| PHASE1 | 1 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT00439062 | PHASE4 | COMPLETED | Treatment of Rheumatoid Arthritis With Roxithromycin |
| NCT04122040 | PHASE3 | COMPLETED | Effects of Roxithromycin on Quality of Life and Physiological Outcomes in Bronchiectasis |
| NCT06798051 | PHASE1 | COMPLETED | Bioequivalence Study of Two Roxithromycin Tablets in Healthy Subjects |
| NCT00197379 | Not specified | UNKNOWN | The Effect of 0.5% Roxithromycin Lotion for Androgenetic Alopecia |
| NCT00621387 | Not specified | COMPLETED | Study of Long-Term Antibiotic Treatment in Reactive Arthritis |
Clinical evidence (CIViC)
No CIViC predictive evidence (expected for non-precision-medicine drugs).
Pharmacology
Pharmacogenomics
No PharmGKB pharmacogenomic data curated for this drug.
Related molecules
Related molecules
Molecules sharing ≥1 of this drug’s curated primary targets, merged from two biobtree sources and ranked by shared-target count, then clinical phase: ChEMBL clinical-stage candidates (development phase ≥2) and PubChem drug-class bioactivity (approved / known drugs acting on the target). Deduplicated by drug name; the drug’s own salt forms are excluded. Note: for a drug with few primary targets a shared-target match can reflect off-target / promiscuous binding rather than the same therapeutic mechanism — the phase ordering surfaces bona-fide therapeutics first.
321 molecules share ≥1 primary target. Top 60 by shared-target count:
| Molecule | Source | Status | Shared targets |
|---|---|---|---|
| AMIODARONE | ChEMBL + PubChem | Phase 4 (approved) | MLNR |
| ATAZANAVIR | ChEMBL + PubChem | Phase 4 (approved) | MLNR |
| CANDESARTAN CILEXETIL | ChEMBL + PubChem | Phase 4 (approved) | MLNR |
| CARVEDILOL | ChEMBL + PubChem | Phase 4 (approved) | MLNR |
| CINACALCET | ChEMBL + PubChem | Phase 4 (approved) | MLNR |
| CLEMASTINE | ChEMBL + PubChem | Phase 4 (approved) | MLNR |
| CLOBETASOL PROPIONATE | ChEMBL + PubChem | Phase 4 (approved) | MLNR |
| CRIZOTINIB | ChEMBL + PubChem | Phase 4 (approved) | MLNR |
| ERYTHROMYCIN | ChEMBL + PubChem | Phase 4 (approved) | MLNR |
| FEDRATINIB | ChEMBL + PubChem | Phase 4 (approved) | MLNR |
| HYDROXYPROGESTERONE CAPROATE | ChEMBL + PubChem | Phase 4 (approved) | MLNR |
| PIMOZIDE | ChEMBL + PubChem | Phase 4 (approved) | MLNR |
| PONATINIB | ChEMBL + PubChem | Phase 4 (approved) | MLNR |
| SORAFENIB | ChEMBL + PubChem | Phase 4 (approved) | MLNR |
| TEGASEROD | ChEMBL + PubChem | Phase 4 (approved) | MLNR |
| TELOTRISTAT ETHYL | ChEMBL + PubChem | Phase 4 (approved) | MLNR |
| ACETOPHENAZINE | ChEMBL | Phase 4 (approved) | MLNR |
| AMPRENAVIR | ChEMBL | Phase 4 (approved) | MLNR |
| ARIPIPRAZOLE | ChEMBL | Phase 4 (approved) | MLNR |
| ASTEMIZOLE | ChEMBL | Phase 4 (approved) | MLNR |
| BAZEDOXIFENE | ChEMBL | Phase 4 (approved) | MLNR |
| BENPERIDOL | ChEMBL | Phase 4 (approved) | MLNR |
| BEPRIDIL | ChEMBL | Phase 4 (approved) | MLNR |
| CANNABIDIOL | ChEMBL | Phase 4 (approved) | MLNR |
| CHLORHEXIDINE | ChEMBL | Phase 4 (approved) | MLNR |
| CHLORPROTHIXENE | ChEMBL | Phase 4 (approved) | MLNR |
| CISAPRIDE | ChEMBL | Phase 4 (approved) | MLNR |
| DULOXETINE | ChEMBL | Phase 4 (approved) | MLNR |
| EBASTINE | ChEMBL | Phase 4 (approved) | MLNR |
| FENTICONAZOLE | ChEMBL | Phase 4 (approved) | MLNR |
| FLUSPIRILENE | ChEMBL | Phase 4 (approved) | MLNR |
| FLUTRIMAZOLE | ChEMBL | Phase 4 (approved) | MLNR |
| GLAFENINE | ChEMBL | Phase 4 (approved) | MLNR |
| INDOCYANINE GREEN ACID FORM | ChEMBL | Phase 4 (approved) | MLNR |
| ISRADIPINE | ChEMBL | Phase 4 (approved) | MLNR |
| LASOFOXIFENE | ChEMBL | Phase 4 (approved) | MLNR |
| NAFARELIN | ChEMBL | Phase 4 (approved) | MLNR |
| NEBIVOLOL | ChEMBL | Phase 4 (approved) | MLNR |
| NIMESULIDE | ChEMBL | Phase 4 (approved) | MLNR |
| NITAZOXANIDE | ChEMBL | Phase 4 (approved) | MLNR |
| NOSCAPINE | ChEMBL | Phase 4 (approved) | MLNR |
| OSIMERTINIB | ChEMBL | Phase 4 (approved) | MLNR |
| PERHEXILINE | ChEMBL | Phase 4 (approved) | MLNR |
| PROPIVERINE | ChEMBL | Phase 4 (approved) | MLNR |
| PYRVINIUM | ChEMBL | Phase 4 (approved) | MLNR |
| REBOXETINE | ChEMBL | Phase 4 (approved) | MLNR |
| RIFAXIMIN | ChEMBL | Phase 4 (approved) | MLNR |
| RIMONABANT | ChEMBL | Phase 4 (approved) | MLNR |
| RITONAVIR | ChEMBL | Phase 4 (approved) | MLNR |
| SERTINDOLE | ChEMBL | Phase 4 (approved) | MLNR |
| SERTRALINE | ChEMBL | Phase 4 (approved) | MLNR |
| SUNITINIB | ChEMBL | Phase 4 (approved) | MLNR |
| TACROLIMUS | ChEMBL | Phase 4 (approved) | MLNR |
| TIPRANAVIR | ChEMBL | Phase 4 (approved) | MLNR |
| TRIFLUOPERAZINE | ChEMBL | Phase 4 (approved) | MLNR |
| VILANTEROL | ChEMBL | Phase 4 (approved) | MLNR |
| VINDESINE | ChEMBL | Phase 4 (approved) | MLNR |
| AZELNIDIPINE | ChEMBL | Phase 3 | MLNR |
| BENIDIPINE | ChEMBL | Phase 3 | MLNR |
| CAMICINAL | ChEMBL | Phase 3 | MLNR |
Related Atlas pages
- Genes: MLNR
- Diseases: bacterial infectious disease
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